2696409-13-7
Chemical Structure
K-757
- CAS No.: 2696409-13-7
- Formula:C32H48NO4P
- Molecular Weight:541.70
IUPAC Name: ((S)-3-cyclopropyl-3-(3-((1-(2-(4,4-dimethylpentyl)-5-methoxyphenyl)piperidin-4-yl)methoxy)phenyl)propyl)phosphinic acid
InChIKey: NVWFVRPJBUNBHL-PMERELPUSA-N
SMILES: COC1=CC=C(CCCC(C)(C)C)C(N2CCC(COC3=CC=CC([C@H](C4CC4)CP(O)(C)=O)=C3)CC2)=C1
Biological Activity: K-757 is an orally active, gut-targeted GPR40 agonist with EC50 values of 2.1 nM, 5.6 nM, 4.2 nM and 166 nM in humans, mice, rats and dogs, respectively. K-757 activates nutrient receptors co-expressed on pancreatic β cells and intestinal enteroendocrine cells. K-757 mediates and induces the secretion of satiety hormones GLP-1 and PYY in multiple in vitro and in vivo models. When used in combination with GPR119 agonist K-833, K-757 acts as a potentiator to elevate circulating levels of satiety hormones. K-757 can be used in the research of type 2 diabetes, weight loss and other related metabolic disorders[1][2].
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K-757 | K-757 is an orally active, gut-targeted GPR40 agonist with EC50 values of 2.1 nM, 5.6 nM, 4.2 nM and 166 nM in humans, mice, rats and dogs, respectively. K-757 activates nutrient receptors co-expressed on pancreatic β cells and intestinal enteroendocrine cells. K-757 mediates and induces the secretion of satiety hormones GLP-1 and PYY in multiple in vitro and in vivo models. When used in combination with GPR119 agonist K-833, K-757 acts as a potentiator to elevate circulating levels of satiety hormones. K-757 can be used in the research of type 2 diabetes, weight loss and other related metabolic disorders. | |||||||||||||||||||||
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References
- [1]. Crutchlow M, et al. Combined GPR40 and GPR119 full agonism with K-757 and K-833 results in robust glucose lowering and modest weight loss in overweight/obese subjects with T2DM. Diabetes Obes Metab. 2025 Nov;27(11):6264-6274.
- [2]. Moyes CR, et al. Discovery of Gut-Targeted GPR40 Agonist K-757 and GPR119 Agonist K-833, a Combination Treatment for Metabolic Disorders. Journal of medicinal chemistry. 2025 Aug 14;68(15):15339-15357. [Content Brief]
